CL 316,243 (disodium salt) |
| Catalog No.GC43276 |
Un agoniste sélectif des récepteurs β3 adrénergiques murins
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Cas No.: 151126-84-0,138908-40-4
Sample solution is provided at 25 µL, 10mM.
EC50: (3.0±0.3) X 10-8 M for β3 adrenoceptor [1].
Benzodioxole-containing phenethanolamine CL-316,243 is a murine-selective β3 adrenoceptor agonist which can correct obesity and elevated blood glucose in diabetic rodents, which offers an exciting possibility for the treatment of non-insulin-dependent diabetes as well as obesity without undesired β-mediated side effects [3]. β3 adrenoceptor is located mainly in adipose tissue and is involved in the regulation of lipolysis and thermogenesis.
In vitro: The compound was a potent stimulant of rat adipocyte lipolysis (β3 effect, EC50 = (3.0±0.3) X 10-8 M), had no effect on the rate of contraction of guinea pig atria (β1 effect, EC50 > 10-4 M), and had only a very limited ability to inhibit insulin-stimulated [14C] glucose incorporation into glycogen in isolated rat soleus muacle (β2 effect, IC50 = (3.0±1.0) X 10-5 M) [1].
In vivo: In rat, CL-316,243 treatment resulted in increased growth rates and significant changes in food consumption at the end of the 10-day treatment period. CL-316,243 treatment increased insulin responsiveness and sensitivity in non-insulin-resistant rodent species. The CL-316,243 induced increases in whole-body glucose disposal were due entirely to increases in adipose tissue glucose uptake, while muscle glucose uptake remained unaltered [2].
Clinical trial: So far, no clinical study has been conducted.
[1]. Bloom, J.D., Dutia, M.D., Johnson, B.D., et al. Disodium (R,R)-5-[2-[[2-(3-chlorophenyl)-2-hydroxyethyl]-amino] propyl]-1,3-benzodioxole-2,2-dicarboxylate (CL 316,243). A potent β-adrenergic agonist virtually specific for β3 receptors. A promising antidiabetic and antiobesity agent. Journal of Medicinal Chemistry 35(16), 3081-3084 (1992).
[2]. Baker, J.G. The selectivity of β-adrenoceptor antagonists at the human β1, β2 and β3 adrenoceptors. Br. J. Pharmacol. 144(3), 317-322 (2005).
[3]. Guerra, C., Koza, R.A., Yamashita, H., et al. Emergence of brown adipocytes in white fat in mice is under genetic control. Effects on body weight and adiposity. Journal of Clinical Investigation 102(2), 412-420 (1998).
[4]. MacPherson, R.E.K., Castellani, L., Bueadoin, M.S., et al. Evidence for fatty acids mediating CL 316,243-induced reductions in blood glucose in mice. American Journal of Physiology.Endocrinology and Metabolism 307(7), E563-E570 (2014).
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